oral BET inhibitor
4.5 mg QD, phase I/II for cancer
from bromodomain-focused HTS, SBDD
Journal of Medicinal Chemistry
Bristol Myers Squibb
BMS-986158
The BMS BET inhibitor, BMS-986158, is in a Ph. I/IIa trial in advanced cancers. During the optimization of the molecule from a carbazole hit, the authors employed a bold scaffold-hopping…